Resveratrol is a non-flavonoid polyphenol having stilbene structure, and is an anti-toxin synthesized by plants under stress. Resveratrol is a natural anti-oxidant that can reduce blood viscosity, inhibit platelet coagulation and improve vasodilation to maintain blood flow; and it can prevent the occurrence and development of cancer, and is effective for the prevention and treatment of atherosclerosis, coronary heart disease, ischemic heart disease, and high blood cholesterol. In addition, resveratrol also has estrogen-like effects, thus can be used for the treatment of breast cancer. Recently, the resveratrol becomes widely useful in pharmaceutical and food industry, and has highly potential value in market. The bioavailability of resveratrol is low, due to its water-insoluble and lipid-insoluble property, which reduces its efficacy and limits its applications.
Phospholipid complex (Phytosome) is a more stable complex formed by a pharmaceutical with a phospholipid through charge transfer between the pharmaceutical and the phospholipid molecule. Phospholipid complex, as a new type pharmaceutical formulation, can significantly improve the lipid-solubility absorption, and bioavailability of the pharmaceutical, and reduce the side effects of the pharmaceutical. Although the phospholipid complex can improve the lipid-soluble index of pharmaceuticals, it is difficult to be dissolved in water, especially when the phospholipid complex is in a form of a formulation of high concentration.
U.S. Patent Application US2004116386A1 disclosed a resveratrol phospholipid complex and a preparation method thereof. Chinese Patent Application Publication No. CN101095664 also disclosed a resveratrol phospholipid complex, its preparation method and applications. According to the disclosure of either of the two patent publications, the resveratrol-phospholipid complex renders lipophilic property to the lipid-insoluble resveratrol, and thus can increase the lipid-soluble index of the resveratrol. However, an aqueous dispersion of the resveratrol-phospholipid complex is not stable because the resveratrol-phospholipid complex is poorly dispersed in water, crystallization of the resveratrol occurs and therefore the resveratrol is easily precipitated from the aqueous dispersion of the complex. These disadvantages limit the application of resveratrol-phospholipid complex in formulating, for example, a resveratrol injection solution, an oral liquid, or a spray formulation for skin care.